U.S. patent application number 10/715915 was filed with the patent office on 2004-05-27 for oral delivery system and method for making same.
Invention is credited to Cooker, John.
Application Number | 20040101540 10/715915 |
Document ID | / |
Family ID | 46300359 |
Filed Date | 2004-05-27 |
United States Patent
Application |
20040101540 |
Kind Code |
A1 |
Cooker, John |
May 27, 2004 |
Oral delivery system and method for making same
Abstract
The present invention is directed to improved oral dosage forms
that are significantly easier to swallow. In accordance with the
present invention, the oral dosage forms are configured to have
relatively greater weight and/or density to effect partial or total
submergence in the liquid with which the oral dosage form is taken.
In one embodiment, the oral dosage form has an active ingredient,
an inactive ingredient, and a digestible substance that has a
predetermined weight that effects at least partial sinking of the
oral dosage form in the liquid. In a preferred embodiment, the
active ingredient and inactive ingredient have a combined total
weight that is substantially less than the predetermined weight of
the digestible substance.
Inventors: |
Cooker, John; (Rohrersville,
MD) |
Correspondence
Address: |
LAW OFFICES OF RAYMOND A. NUZZO, LLC
579 THOMPSON AVENUE
EAST HAVEN
CT
06512
US
|
Family ID: |
46300359 |
Appl. No.: |
10/715915 |
Filed: |
November 18, 2003 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
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10715915 |
Nov 18, 2003 |
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09614243 |
Jul 12, 2000 |
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6656501 |
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60151901 |
Sep 1, 1999 |
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Current U.S.
Class: |
424/400 ;
424/451; 424/452 |
Current CPC
Class: |
A61K 9/4808
20130101 |
Class at
Publication: |
424/400 ;
424/452; 424/451 |
International
Class: |
A61K 009/00; A61K
009/48 |
Claims
1. An oral dosage form for swallowing with liquid, comprising: an
active ingredient; an inactive ingredient; and a digestible
substance having a predetermined weight that effects at least
partial sinking of the oral dosage form in the liquid.
2. The oral dosage form according to claim 1 wherein the active
ingredient and inactive ingredient have a combined total weight
that is substantially less than the predetermined weight of the
digestible substance.
3. The oral dosage form according to claim 1 wherein the percentage
of the total weight of the oral dosage form that is due to the
weight of the digestible substance is between about 5% and 95%.
4. The oral dosage form according to claim 1 wherein the digestible
substance is a filler.
5. The oral dosage form according to claim 4 wherein the filler is
a solid.
6. The oral dosage form according to claim 4 wherein the filler is
a semi-solid.
7. The oral dosage form according to claim 4 wherein the filler is
coated over the active and inactive ingredients.
8. The oral dosage form according to claim 1 wherein the digestible
substance is a binder.
9. The oral dosage form according to claim 1 wherein the oral
dosage form comprises a capsule having a first end and a second
end, and wherein the active and inactive ingredients and the
substance are compressed within the capsule.
10. The oral dosage form according to claim 9 wherein the
digestible substance is concentrated at the first end of the
capsule.
11. The oral dosage form according to claim 10 wherein the
predetermined weight effects sinking of substantially the entire
first end of the capsule in the liquid.
12. The oral dosage form according to claim 10 wherein the capsule
has indicia thereon to indicate the first end of the capsule.
13. The oral dosage form according to claim 9 wherein the
digestible substance is a filler which is molded to the inside of
the capsule.
14. The oral dosage form according to claim 9 wherein the
digestible substance is a filler which is adhered to the inside of
the capsule.
15. The oral dosage form according to claim 1 wherein the active
and inactive ingredients and the digestible substance are
configured to form a tablet having a first portion comprising the
active ingredient and a second portion comprising the digestible
substance.
16. The oral dosage form according to claim 1 wherein the active
and inactive ingredients and the digestible substance are
configured to form a caplet having a first portion comprising the
active and inactive ingredients and a second portion comprising the
digestible substance.
17. The oral dosage form according to claim 1 wherein the
percentage of the total weight of the oral dosage form that is due
to the weight of the digestible substance is between about 5% and
95%.
18. An oral dosage form for ingestion with liquid, comprising: an
active ingredient; an inactive ingredient; and a digestible
substance having a predetermined weight that effects an increase in
the density of the oral dosage form to at least 1.0 g/ml.
19. The oral dosage form according to claim 18 wherein the
percentage of the total weight of the oral dosage form that is due
to the weight of the digestible substance is between about 5% and
95%.
20. The oral dosage form according to claim 19 wherein the
percentage of the total weight of the oral dosage form that is due
to the weight of the digestible substance is between about 15% and
80%.
21. An oral dosage form configured to be swallowed in whole with a
liquid, comprising: a capsule having a first portion and a second
portion attached to the first portion, each portion having an
interior; an active ingredient concentrated in the interior of the
first portion; and a predetermined amount of digestible filler
concentrated in the interior of the second portion of the capsule,
the filler being chosen from the group sucrose, dextrose, lactose,
fructose, microcrystaline cellulose, sorbitol, xylitol, isomalt,
gelatin and starch, the filler having a predetermined weight that
increases the density of the capsule to a predetermined density
that effects sinking of at least the second portion of the capsule
below the surface of the liquid, the amount and concentration of
the filler being such as to eliminate formation of regions within
the interior of the second portion that are relatively low density
with respect to the liquid with which the capsule is swallowed;
wherein the percentage of the total weight of the capsule that is
due to the weight of the filler is between about 5% and 95% and
wherein the amount and concentration of the filler in the interior
of the second portion significantly reduce the buoyancy of the
capsule so as to cause at least the second portion of the capsule
to sink below the surface of the liquid.
22. The oral dosage form according to claim 21 wherein the first
portion of the capsule comprises a body portion of the capsule and
the second portion comprises a cap portion of the capsule.
23. The oral dosage form according to claim 21 wherein the
predetermined weight and concentration of the filler in the second
portion produces a density of the second portion that is at least
1.0 g/ml.
24. An oral dosage form configured to be swallowed in whole with a
liquid, comprising: a body portion having an opening and an
interior; an active ingredient concentrated in the interior of the
body portion; ingredients disposed in the interior of the body
portion; and a plug portion attached to the body portion so as to
seal the opening, the plug portion comprising a predetermined
amount of digestible filler; and wherein the percentage of the
total weight of the oral dosage form that is due to the weight of
the filler is between about 5% and 95% and wherein the amount and
concentration of the filler significantly reduce the buoyancy of
the oral dosage form so as to cause a significant portion of the
oral dosage form to sink below the surface of the liquid.
25. A method for making a density-augmented capsule, comprising:
providing a capsule body portion having an interior for receiving
ingredients; providing a capsule cap portion that has an interior
for receiving a filler substance; retaining the capsule body
portion so that it is substantially stationary; depositing
ingredients into the capsule body portion; depositing a filler
substance into the cap portion; and joining the capsule cap portion
to capsule body portion.
26. The method according to claim 25 wherein the ingredients
include active ingredients.
27. The method according to claim 26 wherein the ingredients
further include inactive ingredients.
28. A tablet for ingestion with a liquid, comprising: a first end;
a second end; an active ingredient; an inactive ingredient; and a
digestible substance having a predetermined density which is
concentrated at the first end so as to effect sinking of at least a
portion of the tablet in the liquid.
29. The oral dosage form according to claim 28 wherein the
percentage of the total weight of the tablet that is due to the
weight of the digestible substance is between about 15% and
80%.
30. The table according to claim 28 wherein the tablet has a
generally conical shape which tapers from the first end to the
second end.
31. The table according to claim 28 wherein the tablet has a
generally trapezoidal shape which tapers from the first end to the
second end.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application is a continuation-in-part and claims the
benefit of commonly owned and copending U.S. application Ser. No.
09/614,243, filed Jul. 12, 2000, which claimed the benefit of
commonly owned U.S. Provisional Application Ser. No. 60/151,901,
filed Sep. 1, 1999.
COPYRIGHT NOTICE
[0002] .COPYRGT. Copyright 2000, 2003 John T. Cooker.
[0003] All rights reserved.
BACKGROUND OF THE INVENTION
[0004] A portion of the disclosure of this patent document contains
material that is subject to copyright protection. The copyright
owner has no objection to the facsimile reproduction by anyone of
the patent document or the patent disclosure, as it appears in the
U.S. Patent and Trademark Office patent file or records, but
otherwise reserves all copyright rights whatsoever.
[0005] 1. Field of the Invention
[0006] The present invention generally relates to an oral delivery
system.
[0007] 2. Description of Related Art
[0008] The pharmaceutical industry has developed a variety of
medications, medicaments, vitamins, nutritional supplements, etc.
(collectively referred to herein as "oral dosages") that can be
taken orally and which are in the form of capsules, tablets, gel
caps and their like (collectively referred to herein as "oral
dosage forms"). However, many consumers have experienced difficulty
in swallowing such oral dosage forms. Specifically, many types of
commercially available oral dosage forms become buoyant on the
liquid with which they are taken. This is especially the case with
capsules which are hardened reservoirs of gelatin filled with
powdered ingredients and air. As a result of such a configuration,
the powdered ingredients and air become bubbles sealed in gelatin.
The buoyancy of the oral dosage forms on the liquid causes
discomfort and creates difficulty in swallowing. Specifically, the
buoyancy characteristic creates the following problems:
[0009] 1) the buoyancy of the oral dosage form works against the
downward motion of swallowing and also reduces control of the oral
dosage form by the tongue and pharynx muscles;
[0010] 2) the dry gelatin outer surface of a capsule or gel cap,
when wetted, quickly becomes sticky and easily adheres to surfaces
it contacts. As a result, the oral dosage form may be left behind
as it follows the liquid down the pharynx and esophagus thereby
requiring successive swallows of additional liquid to flush down
the oral dosage form; and
[0011] 3) a capsule, while floating on the liquid, may move out of
its intended aligned position in which the narrow end of its
cylindrical shape points toward the pharynx and esophagus and as a
result, is swallowed at an uncomfortable angle, possibly becoming
lodged in the process.
[0012] Oral dosage forms that have a cylindrical, oval or
rectangular shape (but not round), and which are not heavy enough
to sink in the liquid with which they are taken may move out of
their aligned position while being propelled by the tongue toward
the pharynx and esophagus thereby being swallowed at an
uncomfortable angle.
[0013] The pharmaceutical industry has attempted to solve these
problems by developing various oral dosage forms that supposedly
have improved swallowabilty. In their attempt to solve the
aforementioned problem relating to swallowability, the
pharmaceutical industry has focused on the size, shape and surface
composition of the capsules, tablets, gel caps, etc. In another
attempt to address the problem of swallowability, the industry
developed and produced cylindrical-shaped tablets which were to
replace round shaped tablets, (i.e. a capsule shaped tablet). One
result of the pharmaceutical industry's attention to this problem
was the development of the gelatin-coated caplets or tablets which
not only addressed the problems relating to swallowability but also
consumers' wariness of capsule tampering. Such a caplet is
disclosed in U.S. Pat. No. 5,314,537. Although the gelatin-coated
caplet has provided improvement in the swallowability of such
caplets, the pharmaceutical industry's attempts to solve this
problem are basically limited to the application of coatings to the
exterior of the caplet, tablet, etc.
[0014] The prior art discloses several oral dosage forms, and drug
delivery devices. Wong et al. U.S. Pat. No. 5,198,229 describes a
fluid-imbibing drug delivery device having a first, low density
such that it floats in the stomach contents for a predetermined
prolonged period of time during which it dispenses a drug or other
active agent to the stomach. This drug delivery device also has a
second, higher density such that the device exits the stomach at
the end of the predetermined prolonged period of time. The drug
delivery device disclosed in Wong et al. has two chambers. One of
these chambers is a buoyancy chamber. Due to the buoyancy chamber,
the Wong et al. drug delivery device, in its first stage, floats on
stomach fluids. The Wong et al. drug delivery device achieves
density by release of air in the outer chamber. Therefore, the drug
delivery device described in Wong et al. certainly cannot
facilitate swallowing if it is configured to float first on
liquids. Sharma et al. U.S. Pat. No. 4,894,233 discloses a drug
delivery system comprising a core material comprising a drug, and a
hydrophobic matrix coating the core. The coating delays hydration
of the drug and masks the taste of the drug. The coating comprises
an emulsifier, an edible fatty acid or wax and a glyceride.
However, the use of fatty acids or waxes significantly increases
the buoyancy of the drug delivery system. Such buoyancy can create
difficulty in swallowing the drug delivery system. Eckenhoff U.S.
Pat. No. 5,098,425 describes a ruminant dispensing device that
comprises a density member or weight means that is dispersed in a
hydrogel member. The dispensing device described in Eckenhoff is a
time released dispenser which uses metals as densifying agents.
Examples of such densifying agents described in Eckenhoff are iron,
iron shot, iron shot coated with iron oxide, iron shot magnesium
alloy, steel, stainless steel, copper oxide, a mixture of cobalt
oxide and iron powder, a mixture of iron and copper oxide and the
like. These metals are passed out of the animal's body. Such metal
densifying agents or weight means are obviously not digestible and
are clearly not suited for use by humans.
[0015] Despite the developments discussed above, consumers still
continue to express desire for oral dosage forms that exhibit
improved swallowability characteristics.
SUMMARY OF THE INVENTION
[0016] It is therefore an object of the present invention to
provide new and improved oral dosage forms that solve the
aforementioned problems. Thus, the present invention is directed to
improved oral dosage forms that are significantly easier to
swallow. In accordance with the present invention, the oral dosage
forms are configured to have relatively greater weight and/or
density to effect partial or total submergence in the liquid with
which the oral dosage form is taken. The oral dosage form has a
size that conforms to a size that can be comfortably swallowed.
[0017] In one embodiment, the present invention is directed to an
oral dosage form for ingestion with liquid, comprising, an active
ingredient, an inactive ingredient, and a substance having a
predetermined weight that effects at least partial sinking of the
oral dosage form in the liquid. In a preferred embodiment, the
substance is digestible. In one embodiment, the substance is a
digestible filler material that is added to the active and inactive
ingredients of the oral dosage form. In such an embodiment, the
filler material is within the interior of the oral dosage form. In
another embodiment, the filler material is added to the exterior of
the oral dosage form. In a preferred embodiment, the filler
material is digestible. In a preferred embodiment, the oral dosage
form is configured so that at least the portion of the oral dosage
form that has the filler (i.e. the weighted end of the oral dosage
form) sinks below the surface of the liquid with which the oral
dosage is taken.
[0018] In another embodiment of the invention, the substance is a
binder that is used to increase the weight and/or density of the
oral dosage form. In a preferred embodiment, the binder is
digestible.
[0019] In accordance with one embodiment of the invention, the oral
dosage form comprises a capsule that has a body portion and a cap
portion, and the filler material is placed in the cap portion. In
accordance with another embodiment of the invention, the oral
dosage form comprises a capsule that has a body portion and a cap
portion and the filler material is placed in the body portion.
Other embodiments of the invention are possible as well. For
example, a relatively heavier, denser or larger amount of active
and inactive ingredients are used to formulate the oral dosage
form. In another example, a combination of a binder and a
relatively heavier, denser or larger amount of ingredient is used
to formulate the oral dosage form.
[0020] In a preferred embodiment, the oral dosage form of the
present invention does not utilize fatty acids, oils or waxes so as
not to cause an increase in the buoyancy of the oral dosage form of
the present invention. In a preferred embodiment, the oral dosage
form of the present invention is configured to substantially
eliminate the formation of any air pockets or air chambers so as to
decrease the buoyancy of the oral dosage form.
[0021] Thus, in one aspect, the present invention is directed to an
oral dosage form for swallowing with liquid, comprising an active
ingredient, an inactive ingredient, and a digestible substance
having a predetermined weight that effects at least partial sinking
of the oral dosage form in the liquid. The active ingredient and
inactive ingredient have a combined total weight that is
substantially less than the predetermined weight of the digestible
substance. In one embodiment, the oral dosage form comprises a
capsule having a first end and a second end, and the active and
inactive ingredients and the digestible substance are compressed
within the capsule. The digestible substance is concentrated at the
first end of the capsule so that when a user desires to ingest the
capsule, the buoyancy of the capsule is substantially reduced and
the capsule is aligned so that the first end of the capsule points
in the direction of the pharynx and the second end of the capsule
points in the direction of the mouth thereby substantially reducing
the probability of the capsule being swallowed at an uncomfortable
angle.
BRIEF DESCRIPTION OF THE DRAWINGS
[0022] The features of the invention are believed to be novel. The
figures are for illustration purposes only and are not drawn to
scale. The invention itself, however, both as to organization and
method of operation, may best be understood by reference to the
detailed description which follows taken in conjunction with the
accompanying drawings in which:
[0023] FIG. 1 is perspective view of a capsule configured in
accordance with one embodiment of the present invention wherein a
filler is added to the capsule.
[0024] FIG. 2 is a perspective view of a capsule in accordance with
another embodiment wherein the capsule has indicia thereon to
indicate the portion of the capsule having concentrated weight.
[0025] FIG. 3 is a perspective view of a capsule configured in
accordance with a further embodiment of the present invention
wherein filler granules are added to the capsule.
[0026] FIG. 4 is a perspective view of a capsule configured in
accordance with yet another embodiment of the present invention
wherein a single piece of filler is added to the capsule.
[0027] FIG. 5 is a perspective view of a capsule configured in
accordance with a further embodiment of the present invention
wherein the filler is attached or adhered to the exterior of the
capsule.
[0028] FIG. 6 is a perspective view of a capsule configured in
accordance with yet another embodiment of the present invention
wherein the filler is molded into one of the capsule portions.
[0029] FIG. 7 is top plan view, partially in cross-section, of a
tablet configured in accordance with one embodiment of the present
invention wherein a tablet is embedded in a filler.
[0030] FIG. 8 is a top plan view, partially in cross-section, of a
softgel configured in accordance with one embodiment of the present
invention wherein a filler is embedded in one portion of the
softgel.
[0031] FIG. 9 is a perspective view of a conical-shaped tablet
configured in accordance with a further embodiment of the present
invention wherein a filler substance is dispersed throughout the
tablet.
[0032] FIG. 10 is a top plan view of a generally trapezoidal-shaped
tablet having filler dispersed throughout the tablet.
[0033] FIGS. 11 and 12 are perspective views of a capsule in
accordance with another embodiment of the present invention wherein
a densifying substance is configured as a plug that is attached to
one end of the capsule.
[0034] FIG. 13 is a perspective view of a capsule in accordance
with another embodiment of the present invention wherein the filler
is located in the cap portion of the capsule.
[0035] FIG. 14 is a table that shows typical commercially available
capsule sizes and corresponding capsule volumes.
[0036] FIG. 15 is a table that shows specific filler weights,
filler volumes and corresponding capsule sizes in accordance with
the present invention.
[0037] FIG. 16 is a standardization table in accordance with the
present invention.
[0038] FIG. 17 is a table that shows new capsule sizes, the amount
of additional filler that can be added to the new capsules and the
resulting total filler weight, in accordance with the present
invention.
[0039] FIGS. 18A, 18B and 18C show a conversion table, in
accordance with the present invention, which shows initial capsule
sizes and various powder density and weights that can be achieved
with each particular initial size capsule, and new capsule sizes
and the various total densities and weights that can be achieved
with each new capsule size.
DETAILED DESCRIPTION OF THE INVENTION
[0040] In describing the preferred embodiments of the present
invention, reference will be made herein to FIGS. 1-18C of the
drawings in which like numerals refer to like,features of the
invention.
[0041] Oral dosage forms have a variety of physical
characteristics. One such physical characteristic is the medium
used for transport. Thus, the present invention teaches a variety
of configurations of oral dosage forms and methods for making these
oral dosage forms, that solve the aforementioned problems and
deficiencies associated with conventional oral dosage forms. The
configurations and methods of the present invention are applicable
to the three major types of oral dosage forms: (1) capsules, (2)
tablets and caplets, and (3) soft-gels.
[0042] It has been found that by increasing the weight of oral
dosage forms, unexpected superior results are achieved in that the
swallowability of the oral dosage forms is significantly improved.
In particular, it has been found that an oral dosage form
configured to have a relatively greater weight than that of a
conventional, but same type, oral dosage form, has significantly
improved swallowability characteristics. Specifically, the
"weighted" oral dosage form results in a significantly greater
gravitational force being exerted upon the oral dosage form which
facilitates direct and relatively quicker passage of the oral
dosage form through the pharynx and into the stomach.
[0043] It has also been found that increasing the density of oral
dosage forms, unexpected superior results are achieved in that the
swallowability of the oral dosage forms is significantly improved.
In particular, it has been found that an oral dosage form
configured to have a relatively greater density than that of a
conventional, but same type, oral dosage form has significantly
improved swallowability characteristics. Specifically, the oral
dosage form having the greater density has significantly less
buoyancy with respect to the liquid which is taken with the oral
dosage form. As is described in the foregoing discussion, it is
buoyancy that resists the swallowing process. Thus, by
significantly reducing buoyancy of the oral dosage form, the
swallowability of the oral dosage form is greatly enhanced.
[0044] It also has been found that increased weight and/or density
concentrated at a particular end or side of an oral dosage form
maintains the oral dosage form in a preferred and intended
alignment by vertically positioning the oral dosage form as it is
swallowed. The heavier end of the oral dosage form is positioned
such that it points generally in the direction of the pharynx and
the lighter end points generally toward the mouth. As a result,
swallowability of the oral dosage form is significantly enhanced
because the probability of the oral dosage form being swallowed at
an uncomfortable angle is significantly reduced.
[0045] In accordance with one embodiment of the invention, the
increased weight and/or density concentrated at a particular end or
side of the oral dosage form of the present invention is such as to
cause the oral dosage form to sink entirely in the liquid which is
taken with the oral dosage form while maintaining the vertical
alignment of the oral dosage form as discussed above. In accordance
with another embodiment of the present invention, the increased
weight and/or density concentrated at a particular end or side of
the oral dosage form of the present invention is such as to cause
the oral dosage form to partially sink in the liquid while
maintaining the vertical alignment of the oral dosage form as
discussed above.
[0046] As described above, in one embodiment of the present
invention, a filler substance is added to the ingredients of the
oral dosage form. The filler may be in solid, semi-solid, liquid or
powder form. Furthermore, the filler may be inactive or may provide
an active function, e.g. digestive aid. The filler can be
formulated from any accepted pharmaceutical excipient materials,
whether soluble or insoluble. Such excipient materials include
sucrose, dextrose, lactose, fructose, microcrystaline cellulose,
calcium carbonate, sorbitol, xylitol, isomalt, gelatin, and
starches. However, it is to be understood that these aforementioned
fillers are just examples and that other types of commercially
available fillers can be used as well. The filler can be added at
any convenient time during the filling process. In one embodiment,
the filler material comprises solid sucrose granules that are added
to the ingredients of an oral dosage form. In another embodiment, a
solid sucrose portion is molded or adhered to the inside of an oral
dosage form. In a further embodiment, the filler is applied as a
relatively thick shell of sorbitol to the oral dosage form.
[0047] In accordance with one embodiment of the present invention,
the filler is located in or at a particular portion of the oral
dosage form so as to provide a weighted portion or a high-density
portion. Thus, the weighted or high-density portion of the oral
dosage form is relatively heavier than the remaining portion of the
oral dosage form thereby causing the weighted or high-density
portion to sink first in the liquid taken with which the oral
dosage form is taken. The oral dosage form becomes vertically
positioned within the liquid as a result of the weighted or
high-density portion sinking first. In a preferred embodiment, the
oral dosage form has indicia thereon to indicate which portion of
the oral dosage form is the weighted portion. In the case of
capsules, the indicia enables a consumer to align the weighted or
heavier portion of the capsule in his or her mouth so as to use the
capsule's cylindrical shape to facilitate correct alignment of the
capsule and movement of the capsule through the throat and into the
esophagus thereby reducing the chance that the oral dosage form
will be swallowed at an angle that causes discomfort. As a result,
confidence is instilled in the consumer when using the oral dosage
form. In one embodiment, color is used as indicia to indicate the
weighted portion of the oral dosage form.
[0048] In accordance with another embodiment of the invention, the
oral dosage form may be configured such that the filler is part of
the medium. In the case of a capsule, the filler is part of the
capsule, either the body portion, cap portion, or both. In another
embodiment, the filler is deposited on or disposed over the
exterior surface of the medium of the oral dosage form. In one such
embodiment, the filler is coated over the exterior surface of the
medium of the oral dosage form. In another embodiment, a filler
coating is applied to the exterior surface of the medium by dipping
the oral dosage form in a liquid filler and then allowing
sufficient time for curing and drying. In a preferred embodiment,
the thickness of such a filler coating is between about 20 and 200
mils, inclusive.
[0049] In a further embodiment, a relatively heavier or denser
diluent is used as an ingredient of the oral dosage form. In
particular, a portion of a powdered diluent used to bulk the volume
of a capsule containing a small dosage of ingredients is replaced
with solid granules in order to increase the weight and/or density.
In one example, rice flour in solid granule form is used. Rice
flour in solid granule form has a relatively greater density or
weight and as a result, can be used in the same available oral
dosage form volume thereby providing a relatively heavier and
denser oral dosage form.
[0050] In another embodiment, a binder is used to provide a
relatively denser oral dosage form. Conventional capsules are
typically filled with free flowing ingredients in powder form.
However, conventional capsules do not use binders to adhere the
free flowing ingredients. In accordance with another embodiment of
the present invention, a binder is mixed with a portion of a
capsule's ingredients in order to provide a significant increase in
the density of the oral dosage form. In one embodiment, a starch
binder is mixed with a portion of ingredients to form solids or
semi-solids which, when dried and combined with the remaining
ingredients, form a relatively high-density oral dosage form. As a
result, a smaller capsule can be used, or a relatively larger
amount of ingredients can be used in the original capsule. This
process of binding a portion of the ingredients of a capsule
requires relatively less effort than producing a complete tablet of
all the ingredients and the resulting oral dosage form still
retains the characteristics of a capsule, e.g. the capsule's shiny,
smooth surface.
[0051] In another embodiment, relatively large amounts of diluent
and binder are combined to form a composition that is used to
formulate a tablet in order to increase the weight and/or density
of the tablet. In another embodiment, a binder and a portion of an
active ingredient or diluent of a capsule are mixed to form a solid
which when dried, is added to the other portions of capsule
ingredients thereby eliminating the need for a filler.
[0052] It is to be understood that any of the aforementioned
methods and techniques of the present invention may be used in any
combination to increase the weight and/or density of an oral dosage
form.
[0053] It is to be understood that for purposes of facilitating
understanding of the present invention, the ensuing description
describes the liquid with which the oral dosage form is taken as
water. However, it is to be understood that other liquids may be
used, e.g. soda, juice, coffee, etc. and that the weight and/or
density of the oral dosage form may have to be increased in
accordance with the present invention to eliminate buoyancy of the
oral dosage form on those types of liquids.
[0054] The instant specification describes inactive ingredients
(e.g. excipients) that are used in the production of oral dosages.
In a preferred embodiment, such excipients are commercially
available accepted pharmaceutical excipient materials. In a most
preferred embodiment, such excipients do not contain fatty acids or
oils or waxes since such substances do increase buoyancy which is
contrary to the objects of the present invention. In order to
facilitate understanding of the present invention, the ensuing
description is divided into separate discussions of each of the
three types of oral dosage forms: (1) capsules, (2) tablets and
caplets, and (3) soft-gels.
[0055] 1) Capsules
[0056] As discussed in the foregoing description, conventional
capsules, in effect, are sealed powder and air which have
significant buoyant characteristics. In accordance with one
embodiment of the present invention, a capsule is provided which is
configured to have a weighted or high-density end portion. At least
the weighted end portion of the capsule sinks below the surface of
the liquid with which the capsule is taken. It has been found that
sinking of at least the weighted end portion of the capsule in the
liquid results in a significant improvement in the swallowability
of the capsule without compromising other characteristics that
consumers find favorable, e.g. shiny, smooth capsule surface. In
accordance with this embodiment of the present invention, capsules
are configured to have a relatively greater weight and/or density
than water (the density of water is 1 g/ml @ 4.degree. Celsius)
without increasing the size of the capsule beyond consumer
preference.
EXAMPLE 1
[0057] A typical conventional capsule of 50 mg of the popular
nutritional supplement zinc contains excipients that weigh 462 mg.
Its total weight is 512 mg in a size 0 capsule with a volume of
0.68 ml and has a density D of 0.512 g/0.68 ml or 0.75 g/ml. Since
the density of this capsule is less than 1 g/ml, it will float on
water. In accordance with the present invention, the density D of
the capsule is increased about 0.29 g/ml by the addition of a solid
sucrose filler weighing 250 mg at 0.1 ml. As a result, the end
product (i.e. the modified capsule) will weigh 762 mg at a volume
of 0.73 ml. Due to compression in the filling process, the capsule
will only expand 0.05 ml. Thus, the density-augmented capsule will
now have a density D equal to 0.762 g/0.73 ml, or 1.04 g/ml. The
density-augmented capsule will sink in the water with which it is
swallowed thereby overcoming the problems associated with capsule
buoyancy discussed in the foregoing description. Specifically, the
density-augmented capsule will significantly reduce the probability
of the capsule moving out of correct alignment and being swallowed
at an uncomfortable angle. It is to be understood that the density
of the density-augmented capsule can be further augmented. However,
in a preferred embodiment, the density augmentation is such that it
does not increase the size of the capsule beyond that which can be
comfortably swallowed by consumers. However, it is to be understood
that in the case of a veterinary application, particular animals
may be able to swallow capsules having a size greater than the size
preferred by consumers.
[0058] In Example 1 in the foregoing description, 250 mg or 32% of
the total weight of the end product is the result of the addition
of the solid sucrose filler. Since the range of capsule weight and
density varies, the amount of the filler needed to achieve the
objects of the present invention will also vary. In a preferred
embodiment, the percentage of the total weight of the oral dosage
form that is due to the weight of the digestible substance is
between about 5% and 90%. In one embodiment, the percentage of the
total weight of the end product that is due to the addition of the
filler ranges between 15% and 80%, inclusive. In another
embodiment, the percentage of the total weight of the end product
that is due to the addition of the filler ranges between 25% and
50%, inclusive, if the filler is used exclusively.
Example 2
[0059] In this example, the 512 mg weight of the conventional
capsule described in Example 1 is significantly increased at the
same volume by exchanging its powdered diluent for solid granules.
Specifically, the 200 mg of rice flour power diluent is replaced by
400 mg of sucrose solid granules. The sucrose solid granules
require the same amount of space but weigh twice as much as the
rice flour diluent. Thus, the weight of the capsule is increased to
712 mg at the same volume with a density D of 0.712 g/0.68 ml or
1.04 g/ml. Thus, the weight-augmented capsule will sink in
water.
Example 3
[0060] In this particular example, a binder is used to produce a
capsule having a relatively greater density. For this particular
example, the conventional zinc capsule described above in Example 1
contains about 112 mg of powder zinc and other excipients and about
400 mg of the rice flour diluent. In this example, increasing the
density of the capsule in accordance with the present invention
comprises the following steps: (a) subtracting 200 mg of the rice
flour diluent, (b) providing 200 mg of dry sorbitol, (c) mixing the
sorbitol with liquid to form a syrup-like binder, (d) mixing the
syrup-like binder with the remaining 200 mg of rice flour, (e)
drying the mixture of the syrup-like binder and the rice flour, (f)
forming granules from the dried mixture, and (g) adding the
granules to the 112 mg of powder zinc and remaining excipients. As
a result, the total capsule weight remains about the same but the
volume of the capsule ingredients (zinc, excipients and binder)
shrinks or decreases 0.2 ml allowing the use of smaller capsule
portions. The density D of the end product will be 0.512 g/0.5 ml
or 1.024 g/ml. This density is more than sufficient to allow the
capsule to sink in water. If water is to be used as the liquid
medium with which the capsule is taken, then it is preferable that
the density of the capsule be increased to a density that is
greater than 1 g/ml so as to effect sinking of substantially the
entire capsule in the water. However, it is to be understood that
the density of the capsule, or of any of the oral dosage forms, can
be increased in accordance with the present invention to effect
sinking of the oral dosage form in other types of liquids, e.g.
soda, juices, coffee, milk, etc.
[0061] In an alternate embodiment of the present invention, filler
is placed in the body portion of the capsule along with the
ingredients. The cap portion is then attached to the body portion.
In such a configuration, the size of the body portion is increased
(e.g. elongated) so as to enable filler and ingredients to fit in
the body portion. In accordance with such an alternate embodiment,
a solid filler of micro-crystalline cellulose or lactose is
inserted into the body portion before the empty capsules are
shipped. In a preferred embodiment, adhering agents are used. In
order to achieve maximum effect, a maximum weight and volume of
filler should be used with a given capsule size thereby creating a
system of standardization of filler sizes and corresponding
increased capsule sizes.
[0062] The following example illustrates the embodiment of the
present invention wherein the filler is placed or positioned in the
cap portion of the capsule.
EXAMPLE 4
[0063] A typical conventional capsule of 50 mg of the popular
nutritional supplement zinc contains excipients that weigh 462 mg.
Its total weight is 512 mg in a size 0 capsule with a volume of
0.68 ml and has a density D of 0.512 g/0.68 ml or 0.75 g/ml. Since
the density of this capsule is less than 1 g/ml, it will float on
water. In accordance with the present invention, the density D of
the cap portion of the capsule is increased from approximately
zero, when it is empty, to about 2.5 g/ml by the addition of a
solid sucrose filler weighing 250 mg at 0.1 ml. As a result, the
cap portion of the end product (i.e. the modified capsule) will
sink below the surface of the water with which the capsule is
ingested thereby overcoming the problems associated with capsule
buoyancy discussed in the foregoing description. Specifically, as a
result of the cap portion sinking in the water, the
density-augmented capsule properly aligns itself such that the
whole capsule is parallel with the esophagus thereby preventing the
capsule from being swallowed at an uncomfortable angle.
Furthermore, the density-augmented capsule travels directly down
the esophagus and is not left behind to stick to the esophagus
surface.
EXAMPLE 5
[0064] A 0.500 ml size #1 capsule is typically used to fill 400 mg
of ingredients. In accordance with this embodiment of the present
invention, the size of the capsule is increased to a size #00 with
a 0.950 ml capacity. The additional 0.450 ml of volume is used for
the filler. When a filler having a density of 1.5 g/ml is used, the
extra 0.450 ml volume would accommodate a filler weighing 675 mg.
Thus, standardization can be achieved for any size capsule.
[0065] In another embodiment of the present invention, a size #00
capsule is configured to have an elongated geometry so as to
provide a further 0.135 ml of volume or 14% increase in space) for
a filler weighing 202 mg. As used herein, the designation "el"
refers to such elongated capsule geometry. Referring to FIG. 14,
there is shown a table that shows typical commercially available
capsule sizes and corresponding capsule volumes. Referring to FIG.
15, there is shown a table that shows specific filler weights,
filler volumes and corresponding increased capsule sizes in
accordance with the present invention. The additional filler
increases the density of the finished capsule to a density that is
substantially close to or above the density of water. Lactose or
micro-crystalline fillers have a density of 1.5 in solid form.
Thus, in accordance with the present invention, FIG. 16 shows a
standardization table for this type of filler (i.e. having a
density of 1.5 in solid form) for each respective capsule size.
Referring to FIG. 17, there is shown a table that shows new capsule
sizes, and the amount of additional filler that can be added to the
new sized capsules and the resulting total filler weight. As shown
in FIGS. 16 and 17, capsule sizes 4 and 5 are increased to size 2.
The difference in a size 5 capsule and a size 2 capsule is 0.24 ml
which will accommodate a filler weight of 360 mg (0.24 ml.times.1.5
mg (solid filler density)). The difference in a size 4 capsule and
a size 2 capsule is 0.16 ml which can accommodate a filler weight
of 0.16 ml.times.1.5 mg=240 mg.
[0066] Referring to FIGS. 18A, 18B and 18C, in accordance with the
present invention, there is shown a conversion table that shows
initial capsule sizes and various powder density and weights that
can be achieved with each particular initial size capsule, and new
capsule sizes and the various total densities and weights that can
be achieved with each new capsule size. As shown in FIGS. 18A, 18B,
and 18C, the various total densities and weights that can be
achieved with each new capsule size are relatively greater than the
densities and weights that are possible for the corresponding
initial capsule sizes. Thus, the table of FIGS. 18A, 18B, and 18C
provides a standardization system which provides seven (7) capsule
sizes that accommodate the standard capsule sizes at four or more
powder densities. Thus, the increase in densities is clearly
demonstrated.
[0067] In order to produce the oral dosage forms in accordance with
the present invention, particular, pertinent and novel
manufacturing steps are implemented. These steps are described in
the ensuing description.
[0068] Capsules typically are comprised of two portions (i.e. body
portion and cap portion) that are pushed together to enclose the
capsule ingredients. The capsule portions are pushed together by
applying a predetermined force. This type of "enclosing" technique
does not employ any steps to seal the capsule portions together
after the predetermined force is applied. However, it has been
found that the force currently being used in conventional processes
to compress the ingredients to an effective density is not
sufficient because the capsule ingredients tend to bounce back when
the capsule portions are not sealed together. The method of the
present invention includes a particular step that pertains to the
application of such force. Specifically, the method of the present
invention includes the step of applying a relatively greater force
to the capsule portions, in comparison to the force applied in
conventional capsule fabrication processes, in order to extract
substantially all of the air from the powdered ingredients. The
extraction of air from the interior of the capsule facilitates
swallowability of the capsule. Furthermore, the increased force
facilitates the positioning of the filler and the ingredients
within the capsule volume.
[0069] In another embodiment of the method of the present
invention, the capsule portion holding the ingredients is
configured to have a deeper well to accommodate the filler
material. This is illustrated in FIG. 1. Capsule 10 generally
comprises cap portion 12 and body portion 14. Body portion 14 holds
the ingredients during the filling process. In one embodiment, body
portion 14 is configured to have a relatively deeper "well" in
order to accommodate filler material or a binder that is used to
increase the weight and/or density of the capsule in accordance
with the present invention. In such an embodiment, the length of
body portion 14 is increased or elongated to accommodate filler
material or binders. In another embodiment, the length of cap
portion 12 is increased or elongated to accommodate filler material
or binders. In yet a further embodiment, the diameter of portions
12 and 14 are increased to accommodate larger amounts of filler
materials or binders.
[0070] The filler may be configured to have any suitable shape.
However, it has been found that if a single piece of solid filler
is used in a capsule, then the preferred shape of the solid filler
should be generally spherical or oval in order to facilitate
compacting powder ingredients and filling air gaps. In one
embodiment, the filler is covered with a film material that
prevents it from interacting with the ingredients.
[0071] In a further embodiment of the method of the present
invention, the capsule components, e.g. portions 12 and 14, are
formulated to have a relatively greater thickness to provide
relatively greater strength to withstand the greater force
resulting from addition of the filler. Furthermore, it is to be
understood that the added thickness of the capsule portions also
contributes to the increase in weight and density of the capsule in
accordance with the present invention.
[0072] In another embodiment of the method of the present
invention, a sealing process is used to hold the joined capsule
portions in place. Specifically, this sealing process comprises the
step of applying an adhering agent around the seam of the filled
and joined capsule portions.
[0073] In a further embodiment, a locking process is used to hold
the joined capsule portions in place. In such a process,
indentations or moldings are formed on the capsule cap and body.
The indentations or moldings are used to lock the cap and body
together. A plurality of indentations or moldings can be used to
provide capsules of varying lengths.
[0074] In yet another embodiment of the method of the present
invention, when the weight of the capsule is increased to improve
swallowability, as described above, the weight is concentrated at
one end of the capsule. When such a configuration is used, markings
or indicia are applied to the weighted portion of the capsule so as
to indicate the weighted portion of the capsule. Such a
configuration is shown in FIG. 2. Capsule 20 comprises cap portion
22 and body portion 24. Portion 22 has indicia 26 to indicate that
portion 22 is the weighted portion and that capsule 20 should
placed in the consumer's mouth so that weighted portion 22 is
pointing toward the opening of the esophagus. In one embodiment,
the indicia 26 consist of a color. However, it is to be understood
that other types of indicia can be used, e.g. letters, numbers,
etc.
[0075] Referring to FIG. 3, as described in the foregoing
description, granules of a particular substance, e.g. sucrose solid
granules, are added to the capsule to increase the weight and/or
density of the capsule. Thus, in this embodiment of the method of
the present invention, the method comprise the steps of (a)
providing capsule 30 that comprises capsule portions 32 and 34, (b)
retaining portion 34 so that it is stationary, (c) depositing
ingredients 35 into portion 34, (d) depositing granules 36 into
portion 34, and (e) joining capsule portions 32 and 34 together. In
another embodiment, this particular method includes the step of
applying indicia to the weighted portion of capsule 30 in a manner
described above.
[0076] Referring to FIG. 4, the method of the present invention
also provides particular steps for using a single piece of filler
substance. Specifically, these particular steps comprise (a)
providing capsule 40 that comprises cap portion 42 and body portion
44, (b) retaining body portion 44 so that it is stationary, (c)
depositing ingredients 45 into body portion 44, (d) depositing
single filler substance 46 into body portion 44, and (e) joining
cap portion 42 to body portion 44. In one embodiment, single filler
substance 46 is deposited into body portion 44 by capsule filling
machines known in the industry. In one embodiment, this method
includes the step of applying indicia to the weighted portion of
capsule 40 in a manner as described above. In one embodiment, the
predetermined weight and concentration of the filler in portion 44
produces a density of portion 44 that is at least 1.0 g/ml.
[0077] In a further embodiment of the present invention, a capsule
is configured to have a body portion (e.g. portion 44) that is
sized to contain the active ingredients, any required inactive
ingredients, and the filler, and a flat cap portion (not shown)
that is used to seal the body portion thereby substantially
eliminating any air pockets or air reservoir.
[0078] Referring to FIG. 5, in another embodiment of the method of
the present invention, a method is provided for adding or attaching
a filler to the exterior of either capsule portion. Specifically,
this method comprises the steps of (a) providing capsule 60 that
comprises capsule portions 62 and 64, (b) retaining portion 64 so
that it is stationary, (c) depositing ingredients 66 into portion
64, (d) adhering or attaching filler substance 68 to the exterior
surface of portion 62; and (e) joining capsule portions 62 and 64
together.
[0079] Referring to FIG. 6, in a further embodiment of the method
of the present invention, a method is provided for molding a filler
substance into either of the capsule portions. Specifically, this
method comprises the steps of (a) providing capsule 80 that
comprises capsule portions 82 and 84, (b) retaining portion 84 so
that it is stationary, (c) depositing ingredients 86 into portion
84, (d) molding filler substance 88 into portion 82, and (e)
joining capsule portions 82 and 84 together. In an alternate
embodiment of this method, the filler substance 88 is adhered to
the inside of either of the capsule portions. In another
embodiment, the body portion or cap portion, or both, are molded to
have a portion comprised of the filler substance. In a further
embodiment of the present invention, one or both of the capsule
portions are formed from the filler substance. Thus, in such an
embodiment, the entire capsule, i.e. both body and cap portions,
are made from the filler substance.
[0080] Referring to FIG. 13, there is shown a further embodiment of
the present invention. Density-augmented capsule 400 comprises body
portion 402 having an interior for containing ingredients 403 (e.g.
active ingredients and any inactive ingredients), and cap portion
404 having an interior 405 for receiving filler substance 406
(shown in phantom). Filler 406 can be in solid, semi-solid or paste
form. Preferably, filler substance is digestible. Thus, in
accordance with the invention and the embodiment shown in FIG. 13,
the following method is provided (a) providing capsule 400 that
comprises capsule body portion 402 and cap portion 404 which has
interior 405, (b) retaining body portion 402 so that it is
stationary, (c) depositing ingredients 403 into the interior of
body portion 402, (d) depositing filler substance 406 into interior
405 of cap portion 404, and (e) joining cap portion 404 to body
portion 402.
[0081] In another embodiment of the present invention, the solid or
semi-solid filler is placed or positioned only in the interior of
the body portion of the capsule. In a further embodiment, solid or
semi-solid filler is placed in both the interiors of the cap and
body portions of the capsule.
[0082] In yet another embodiment, a capsule is configured to
comprise a body portion for containing the active ingredients and a
plug portion. The plug portion is formed from a filler substance.
The filler substance can be in solid form or paste form. This
embodiment is shown in FIGS. 11 and 12. Capsule 300 comprises body
portion 302 and plug portion 304. Body portion 302 has an opening
306 and contains the active ingredients. Plug portion 304 is formed
from the filler and is inserted into opening 306. The size of plug
portion 304 is chosen so as to create a frictional fit between the
plug portion 304 and body portion 302. The amount of active
ingredients and the size of plug portion 304 are chosen so as to
substantially eliminate air pockets within capsule 300. In a
further embodiment, body portion 302 is elongated or lengthened, in
comparison to conventional capsule body portions, so as to
accommodate the active ingredients and plug portion 304. Plug
portion 304 can be plugged or inserted into body portion 302 by
mechanical means such as typical capsule filling machines which are
known in the industry. An advantage of capsule 300 is that plug
portion 304 renders a typical gelatin cap unnecessary.
[0083] The solid filler described above can be standardized in
order to facilitate automated manufacturing processes. The solid
filler can be adhered to the inside of the cap portion of the
capsule while the cap portion is still empty. Capsules typically
are manufactured in standard sizes so that they may be handled by
automatic filling machines.
[0084] The feature of concentrating the filler at one end of the
capsule provides many advantages. One such advantage is that the
end of the capsule having the filler becomes submerged in the
liquid even if the total density of the capsule does not exceed
that of water. This advantage results from the proportionally
larger weight of the "filler end" of the capsule. Even if the
lighter end of the capsule having the powder ingredients still
floats, the effectiveness of the capsule of the present invention
is still achieved by the weighted filler end of the capsule being
submerged. Another advantage is the improved swallowability of the
capsule. A further advantage is that the proportionally larger
weight of the filler end of the capsule counteracts the buoyancy
caused by air bubbles that may be created when the cap portion of
the capsule is joined with the body portion.
[0085] In a further embodiment, the cap portion of the capsule is
configured so as to substantially degrade the formation of any
bubbles therein when the cap portion of the capsule is joined with
the body portion. In one embodiment, this is achieved by
configuring the end of the cap portion to have a generally flat
geometry rather than a curved or rounded end. In another
embodiment, the interior portion of the cap portion that is
adjacent to the end of the cap portion is filled in with the same
material used to formulate the cap portion.
[0086] 2) Tablets and Caplets
[0087] In accordance with the present invention, tablets and
caplets are produced with relatively greater weight and density to
improve swallowability of the tablets and/or caplets. The increase
in weight and density is accomplished by adding a filler as
described above. In one embodiment, the filler is added to the
ingredients. For example, in one embodiment, a solid sucrose filler
is molded in with the ingredients. In another example, the filler
is embedded within the tablet ingredients.
[0088] In another embodiment, the tablet or caplet is configured
such that the active ingredients and any inactive ingredients are
embedded in a filler substance. This example is illustrated in FIG.
7. Tablet 90 comprises portions 92 and 94. Portion 92 is comprised
only of filler. Portion 94 is embedded within the filler. Portion
94 comprises the active ingredients and any inactive
ingredients.
[0089] In yet another embodiment, the tablet is configured such
that one side, end or portion of the tablet has concentrated weight
and has indicia to indicate which side, end or portion has the
concentrated weight.
[0090] In a further embodiment, increasing the weight and density
of the tablet or caplet is accomplished by increasing a component
of the tablet or caplet. In one embodiment, this is accomplished by
increasing the weight of an excipient such as the binder
ingredient.
[0091] In a preferred embodiment, the percentage of the total
weight of the end product that is due to the addition of the
filler, or the increase in the weight of the component, is between
about 15% and 90%, inclusive. More preferably, the percentage of
the total weight of the end product due to the addition of the
filler or increase in the weight of the component is between about
25% and 75%, inclusive. For example, 50% of the weight of a 400 mg
tablet augmented with 200 mg of filler is the result of adding the
filler. In this example, the original weight of the tablet has been
doubled or increased about 100%.
[0092] The increase in weight and/or density provides significantly
improved swallowability of particularly light, small sized tablets
and caplets (i.e. under 300 mg, {fraction (4/10)} ml).
[0093] Referring to FIGS. 9 and 10, there are shown alternate
embodiments of the tablets and caplets of the present invention.
These embodiments utilize a particular shape having a swelled end
which is substantially larger than the opposite end. For example,
FIG. 9 shows a conical-shaped tablet or caplet 200 which has
swelled or enlarged end 202 and a relatively narrow end 204. Filler
206 is dispersed throughout tablet or caplet 200. FIG. 10 shows a
generally-trapezoidal shaped tablet or caplet 208 which has a
swelled or enlarged end 210 and a relatively narrow end 212.
Similarly, filler 214 is dispersed throughout the tablet or caplet
208. As a result of the shape of tablets or caplets 200 and 208,
swelled ends 202 and 210, respectively, are substantially heavier
than the opposite narrow ends. Thus, the swelled or enlarged ends
sink in the liquid with which the tablet or caplet is taken thereby
effecting correct alignment of the tablet or caplet and movement of
the tablet or caplet through the throat and into the esophagus.
[0094] 3) Softgels
[0095] In accordance with the present invention, the weight of
softgels is increased to improve swallowability thereof. In one
embodiment of the present invention, increasing the weight of
softgels is accomplished by the addition of a filler substance.
Specifically, the filler is added to the ingredients, e.g. a solid
sucrose portion. This is illustrated in FIG. 8. Softgel 100
comprises portions 102 and 104. Portion 102 is comprised only of
ingredients. Portion 104 includes filler 106. In one embodiment,
filler 106 is comprised of solid sucrose.
[0096] In another embodiment of the present invention, increasing
the weight of softgels is accomplished by increasing the amount of
a component. For example, if the component is a liquid excipient,
then the amount of the excipient is increased. Increasing the
amount of the component can also be realized by increasing the size
or thickness of the softgel.
[0097] In another embodiment, the softgels can be configured so
that one side or portion of the softgel has concentrated weight and
has indicia to indicate this end.
[0098] In a preferred embodiment, the percentage of total weight of
the softgel that is due to the addition of the filler or increase
in component is between about 15% and 90%, inclusive. More
preferably, the percentage of total weight of the softgel that is
due to the addition of the filler or increase in component is
between about 25% and 75%, inclusive.
[0099] The increase in weight and/or density provides significantly
improved swallowability of particularly light, small sized softgels
(i.e. under 300 mg, {fraction (4/10)} ml).
[0100] Gravity plays a significant role in the process of
swallowing food. The role of gravity in swallowing food is
described in The Human Body, Volume on "Digestion", pp. 60-61,
Torstar Books, 1984 and in The ABC's of the Human Body, Reader's
Digest General Books, page 240, 1987. The relatively greater weight
and/or density of the oral dosage forms of the present invention
effect augmentation of the gravitational force that facilitates the
downward passage of the oral dosage forms. Thus, the swallowability
of the oral dosage forms is significantly increased.
[0101] Thus, the present invention provides new and improved oral
dosage forms that:
[0102] a) solve the aforementioned problems discussed above that
relate to the swallowability of oral dosage forms;
[0103] b) can be provided in the form of capsules, tablets, gelcaps
and softgels;
[0104] c) interact with gravity to facilitate prompt and direct
movement of the oral dosage form to the opening of and through the
esophagus;
[0105] d) results in a relatively faster dissolution rate of the
oral dosage form and relatively faster absorption rate of the
medication provided by the oral dosage form;
[0106] e) can be produced with commercially available ingredients;
and
[0107] f) can be produced without exorbitant manufacturing
costs.
[0108] The principles, preferred embodiments and modes of operation
of the present invention have been described in the foregoing
specification. The invention which is intended to be protected
herein should not, however, be construed as limited to the
particular forms disclosed, as these are to be regarded as
illustrative rather than restrictive. Variations in changes may be
made by those skilled in the art without departing from the spirit
of the invention. Accordingly, the foregoing detailed description
should be considered exemplary in nature and not limited to the
scope and spirit of the invention as set forth in the attached
claims.
[0109] Thus, having described the invention, what is claimed
is:
* * * * *